KR20220109406A - Ras 억제제 - Google Patents

Ras 억제제 Download PDF

Info

Publication number
KR20220109406A
KR20220109406A KR1020227018683A KR20227018683A KR20220109406A KR 20220109406 A KR20220109406 A KR 20220109406A KR 1020227018683 A KR1020227018683 A KR 1020227018683A KR 20227018683 A KR20227018683 A KR 20227018683A KR 20220109406 A KR20220109406 A KR 20220109406A
Authority
KR
South Korea
Prior art keywords
optionally substituted
membered
alkyl
hydrogen
heterocycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
KR1020227018683A
Other languages
English (en)
Korean (ko)
Inventor
제임스 아겐
지. 레슬리 버넷
제니퍼 피첸
아드리안 엘. 길
엘레나 에스. 콜툰
제임스 크레그
안드레아스 부클
앤 브이. 에드워즈
크리스토퍼 셈코
미카 제임스 글리엣
존 이. 녹스
윌리엄 디. 토마스
Original Assignee
레볼루션 메디슨즈, 인크.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 레볼루션 메디슨즈, 인크. filed Critical 레볼루션 메디슨즈, 인크.
Priority to KR1020257028720A priority Critical patent/KR20250133996A/ko
Publication of KR20220109406A publication Critical patent/KR20220109406A/ko
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46—Oxygen atoms
    • C07D213/50—Ketonic radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020227018683A 2019-11-04 2020-11-04 Ras 억제제 Pending KR20220109406A (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020257028720A KR20250133996A (ko) 2019-11-04 2020-11-04 Ras 억제제

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201962930406P 2019-11-04 2019-11-04
US62/930,406 2019-11-04
US201962951562P 2019-12-20 2019-12-20
US62/951,562 2019-12-20
US202063000355P 2020-03-26 2020-03-26
US63/000,355 2020-03-26
US202063043523P 2020-06-24 2020-06-24
US63/043,523 2020-06-24
PCT/US2020/058817 WO2021091967A1 (en) 2019-11-04 2020-11-04 Ras inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020257028720A Division KR20250133996A (ko) 2019-11-04 2020-11-04 Ras 억제제

Publications (1)

Publication Number Publication Date
KR20220109406A true KR20220109406A (ko) 2022-08-04

Family

ID=73646455

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020227018683A Pending KR20220109406A (ko) 2019-11-04 2020-11-04 Ras 억제제
KR1020257028720A Pending KR20250133996A (ko) 2019-11-04 2020-11-04 Ras 억제제

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020257028720A Pending KR20250133996A (ko) 2019-11-04 2020-11-04 Ras 억제제

Country Status (17)

Country Link
US (2) US11739074B2 (de)
EP (2) EP4054720A1 (de)
JP (1) JP7823816B2 (de)
KR (2) KR20220109406A (de)
CN (4) CN121471132A (de)
AU (2) AU2020379731A1 (de)
BR (1) BR112022008534A2 (de)
CA (1) CA3159559A1 (de)
CL (2) CL2023000973A1 (de)
CO (1) CO2022006030A2 (de)
CR (1) CR20220240A (de)
IL (2) IL322454A (de)
MX (1) MX2022005357A (de)
PE (1) PE20221277A1 (de)
PH (1) PH12022550973A1 (de)
TW (1) TW202132315A (de)
WO (1) WO2021091967A1 (de)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
SG11201906412SA (en) 2017-01-23 2019-08-27 Revolution Medicines Inc Pyridine compounds as allosteric shp2 inhibitors
BR112019015075A2 (pt) 2017-01-23 2020-03-10 Revolution Medicines, Inc. Compostos bicíclicos como inibidores de shp2 alostéricos
SG11202002941WA (en) 2017-10-12 2020-04-29 Revolution Medicines Inc Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
CA3084058A1 (en) 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
ES3004338T3 (en) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
KR102871791B1 (ko) 2018-09-10 2025-10-15 미라티 테라퓨틱스, 인크. 병용 요법
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
CA3148745A1 (en) 2019-08-29 2021-03-04 Xiaolun Wang Kras g12d inhibitors
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
WO2021067326A1 (en) * 2019-10-01 2021-04-08 Bristol-Myers Squibb Company Substituted bicyclic heteroaryl compounds
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
PE20221277A1 (es) 2019-11-04 2022-09-05 Revolution Medicines Inc Inhibidores de ras
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
KR20230042600A (ko) * 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
US12286431B2 (en) 2020-09-11 2025-04-29 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
AU2021345111B2 (en) 2020-09-15 2025-11-27 Revolution Medicines, Inc. Indole derivatives as Ras inhibitors in the treatment of cancer
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (de) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidin-pan-kras-hemmer
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
CA3203205A1 (en) 2021-01-19 2022-07-28 Mandar Ramesh Bhonde Pharmaceutical combinations of sos1 inhibitors for treating and/or preventing cancer
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
EP4334324A1 (de) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Kovalente ras-inhibitoren und verwendungen davon
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
MX2023013912A (es) 2021-05-25 2024-02-12 Revolution Medicines Inc Metodos para inhibir ras.
WO2023015559A1 (en) * 2021-08-13 2023-02-16 Nutshell Biotech (Shanghai) Co., Ltd. Macrocycle compounds as inhibitors of ras
AR126854A1 (es) * 2021-08-27 2023-11-22 Hoffmann La Roche Compuestos macrocíclicos para el tratamiento de cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023086341A1 (en) * 2021-11-09 2023-05-19 Biomea Fusion, Inc. Inhibitors of kras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CA3246887A1 (en) * 2022-01-10 2023-07-13 Revolution Medicines, Inc. RAS INHIBITORS
EP4227307A1 (de) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazinverbindungen als shp2-inhibitoren
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
TW202400607A (zh) * 2022-04-25 2024-01-01 美商翰森生物有限責任公司 環狀化合物、製備方法及其醫藥用途
EP4532503A1 (de) * 2022-06-01 2025-04-09 F. Hoffmann-La Roche AG Makrocyclische haloindolverbindungen zur behandlung von krebs
AU2023285116A1 (en) * 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4551295A1 (de) * 2022-07-08 2025-05-14 F. Hoffmann-La Roche AG Makrocyclische verbindungen als kras-hemmer
EP4582426A4 (de) * 2022-09-19 2025-12-24 Adlai Nortye Biopharma Co Ltd Pan-kras-inhibitorverbindung
CN117720556B (zh) * 2022-09-19 2026-05-05 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物及其制备方法和用途
AU2023350264A1 (en) 2022-09-29 2025-04-10 Guangzhou Joyo Pharmatech Co., Ltd Macrocyclic derivative and use thereof
CN120659773A (zh) 2022-11-09 2025-09-16 锐新医药公司 化合物、复合物以及其制备方法和用途
LU505465B1 (en) * 2022-11-16 2024-05-14 Adlai Nortye Biopharma Co Ltd A pan-KRAS inhibitor compound
CN117534684A (zh) * 2022-11-29 2024-02-09 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
WO2024149819A1 (en) * 2023-01-13 2024-07-18 F. Hoffmann-La Roche Ag Sulfonylvinyl compounds for the treatment of cancer
CN120615093A (zh) * 2023-01-19 2025-09-09 劲方医药科技(上海)股份有限公司 大环化合物及其制法和用途
CR20250329A (es) 2023-02-14 2025-09-12 Hoffmann La Roche Compuestos tricíclicos para el tratamiento del cáncer
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
EP4688790A1 (de) 2023-04-07 2026-02-11 Revolution Medicines, Inc. Makrocyclische ras-inhibitoren
CN121487922A (zh) 2023-04-14 2026-02-06 锐新医药公司 Ras抑制剂的合成
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
CN121013851A (zh) * 2023-04-27 2025-11-25 晨晖生物科技(香港)有限公司 大环化合物及其治疗用途
CN121712509A (zh) 2023-05-04 2026-03-20 锐新医药公司 用于ras相关疾病或病症的组合疗法
EP4720059A1 (de) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclische verbindungen und verwendungen davon
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250115551A1 (en) 2023-10-03 2025-04-10 Revolution Medicines, Inc. Synthesis of ras inhibitors
AU2024358992A1 (en) 2023-10-09 2026-04-23 Incyte Corporation Combination comprising a kras g12d inhibitor and an egfr inhibitor for use in the treatment of cancer
WO2025080593A1 (en) 2023-10-09 2025-04-17 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
IL327306A (en) 2023-10-12 2026-05-01 Revolution Medicines Inc Macrocyclic RAS inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2025261498A1 (zh) * 2024-06-21 2025-12-26 晨晖生物科技(香港)有限公司 大环化合物及其合成方法和应用
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026021499A1 (zh) * 2024-07-24 2026-01-29 苏州泽璟生物制药股份有限公司 卤代亚烷基取代环烷基或杂环基类抑制剂及其制备方法和应用
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026073180A2 (en) * 2024-09-30 2026-04-02 Revolution Medicines, Inc. Synthesis of ras inhibitors
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090323A1 (en) 2024-10-23 2026-04-30 Incyte Corporation Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor and its use in the treatment of cancer
WO2026090333A1 (en) 2024-10-23 2026-04-30 Incyte Corporation Combination using a kras g12d inhibitor and chemotherapy combinations as well as their use in the treatment of cancer

Family Cites Families (321)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CY1915A (en) 1984-10-04 1985-09-27 Sandoz Ag Cyclosporins
EP0194972B1 (de) 1985-03-11 1992-07-29 Sandoz Ag Cyclosporine
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5858358A (en) 1992-04-07 1999-01-12 The United States Of America As Represented By The Secretary Of The Navy Methods for selectively stimulating proliferation of T cells
US6352694B1 (en) 1994-06-03 2002-03-05 Genetics Institute, Inc. Methods for inducing a population of T cells to proliferate using agents which recognize TCR/CD3 and ligands which stimulate an accessory molecule on the surface of the T cells
US6905680B2 (en) 1988-11-23 2005-06-14 Genetics Institute, Inc. Methods of treating HIV infected subjects
US6534055B1 (en) 1988-11-23 2003-03-18 Genetics Institute, Inc. Methods for selectively stimulating proliferation of T cells
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
DK0393934T3 (da) 1989-04-15 1994-11-21 Nippon Chemiphar Co Nye peptider samt antidemensmidler indeholdende disse peptider
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
CA2102780C (en) 1991-05-10 2007-01-09 Alfred P. Spada Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
ES2089723T3 (es) 1992-03-27 1996-10-01 American Home Prod 29-demetoxirapamicina para inducir la inmunodepresion.
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
DE4221054A1 (de) 1992-06-30 1994-01-05 Herbst Bremer Goldschlaegerei Präparat zur prophylaktischen und therapeutischen Behandlung von Karies sowie Verfahren zum Herstellen desselben
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
PT669929E (pt) 1992-11-13 2007-04-30 Immunex Corp Ligando de elk, uma citoquina
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
ES2164713T3 (es) 1993-09-20 2002-03-01 Univ Leland Stanford Junior Produccion recombinante de nuevos poliquetidos.
JPH08503971A (ja) 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
PT734389E (pt) 1993-12-17 2000-09-29 Novartis Ag Derivados de rapamicina uteis como imunossupressores
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
IL112873A (en) 1994-03-08 2005-03-20 Wyeth Corp Rapamycin-fkbp12 binding proteins, their isolation and their use
AU702522B2 (en) 1994-04-15 1999-02-25 Amgen, Inc. HEK5, HEK7, HEK8, HEK11, new EPH-like receptor protein tyrosine kinases
DE59500788D1 (de) 1994-05-03 1997-11-20 Ciba Geigy Ag Pyrrolopyrimidinderivate mit antiproliferativer Wirkung
GB9410142D0 (en) 1994-05-20 1994-07-06 Univ Warwick Carbapenems
US7175843B2 (en) 1994-06-03 2007-02-13 Genetics Institute, Llc Methods for selectively stimulating proliferation of T cells
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
GB9524630D0 (en) 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
JP4249804B2 (ja) 1995-04-03 2009-04-08 ノバルティス・アクチエンゲゼルシャフト ピラゾール誘導体およびその製造法
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US7067318B2 (en) 1995-06-07 2006-06-27 The Regents Of The University Of Michigan Methods for transfecting T cells
US6692964B1 (en) 1995-05-04 2004-02-17 The United States Of America As Represented By The Secretary Of The Navy Methods for transfecting T cells
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
CZ292233B6 (cs) 1995-06-09 2003-08-13 Novartis Ag Deriváty rapamycinu a jejich použití jako léčiv
US5624677A (en) 1995-06-13 1997-04-29 Pentech Pharmaceuticals, Inc. Controlled release of drugs delivered by sublingual or buccal administration
US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
EP0836605B1 (de) 1995-07-06 2002-02-06 Novartis AG Pyrolopyrimidine und verfahren zu ihrer herstellung
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
AU1441497A (en) 1996-01-23 1997-08-20 Novartis Ag Pyrrolopyrimidines and processes for their preparation
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6051577A (en) 1996-03-15 2000-04-18 Novartis Ag N-7-heterocyclyl pyrrolo[2,3-D]pyrimidines and the use thereof
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
EP0907642B1 (de) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituierte triicyclische derivate zur behandlung hyperproliferativer krankheiten
DK0910633T3 (da) 1996-07-05 2010-03-29 Biotica Tech Ltd Hybrid polyketidsyntase I-gen
US6258823B1 (en) 1996-07-12 2001-07-10 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
EP0818442A3 (de) 1996-07-12 1998-12-30 Pfizer Inc. Cyclische Sulphonderivate als Metalloproteinase-Inhibitoren und zur Hemmung der Produktion von Tumornekrosefaktor
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd., Greenford Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
CA2260898C (en) 1996-07-18 2002-05-14 Pfizer Limited Phosphinate based inhibitors of matrix metalloproteases
DE69738749D1 (de) 1996-08-16 2008-07-17 Schering Corp Zelloberflächen-antigen aus säugetieren und verwandte reagenzien
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
AU720429B2 (en) 1996-08-23 2000-06-01 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
SE9603465D0 (sv) 1996-09-23 1996-09-23 Astra Ab New compounds
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
ES2239779T3 (es) 1996-10-02 2005-10-01 Novartis Ag Derivados de pirimidina y procedimientos para la preparacion de los mismos.
AU4779897A (en) 1996-10-02 1998-04-24 Novartis Ag Fused pyrazole derivatives and processes for their preparation
EP0837063A1 (de) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazolinderivate
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
DE69730151T2 (de) 1997-01-06 2005-08-04 Pfizer Inc. Cyclische sulfonderivate
AU721748B2 (en) 1997-02-03 2000-07-13 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
KR20000070751A (ko) 1997-02-05 2000-11-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 피리도[2,3-ｄ]피리미딘 및 4-아미노피리미딘
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
WO1998034918A1 (en) 1997-02-11 1998-08-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6902913B2 (en) 1997-04-30 2005-06-07 Kosan Biosciences, Inc. Recombinant narbonolide polyketide synthase
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
WO1999007701A1 (en) 1997-08-05 1999-02-18 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
ID23668A (id) 1997-08-08 2000-05-11 Pfizer Prod Inc Turunan asam ariloksiarilsulfonilamino hidroksamat
WO1999020758A1 (en) 1997-10-21 1999-04-29 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6153383A (en) 1997-12-09 2000-11-28 Verdine; Gregory L. Synthetic transcriptional modulators and uses thereof
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
ES2324846T3 (es) 1998-03-04 2009-08-17 Bristol-Myers Squibb Company Inhibidores de la proteina tirosina quinasa de imidazopirazina heterociclo-sustituida.
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
ATE473759T1 (de) 1998-05-22 2010-07-15 Univ Leland Stanford Junior Bifunktionelle moleküle sowie darauf basierende therapien.
IL139934A0 (en) 1998-05-29 2002-02-10 Sugen Inc Pyrrole substituted 2-indolinone derivatives and pharmaceutical compositions containing the same
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
EP1109555A4 (de) 1998-08-31 2001-11-21 Merck & Co Inc Neue angiogeneseinhibitoren
NZ510819A (en) 1998-10-02 2004-03-26 Kosan Biosciences Inc Polyketide synthase enzymes and recombinant DNA constructs therefor
US6686454B1 (en) 1998-10-09 2004-02-03 Isotechnika, Inc. Antibodies to specific regions of cyclosporine related compounds
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
EP1153124A2 (de) 1999-02-09 2001-11-14 The Board Of Trustees Of The Leland Stanford Junior University Verfahren zur modulierung der effizienz von polyketide syntase modulen
JP4673977B2 (ja) 1999-03-30 2011-04-20 ノバルティス アーゲー 炎症性疾患治療用フタラジン誘導体
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
ATE324444T1 (de) 1999-06-07 2006-05-15 Immunex Corp Tek-antagonisten
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
PT1196186E (pt) 1999-07-12 2008-02-14 Genentech Inc Promoção ou inibição da angiogénese e da cardiovascularização com homólogos de ligandos/receptores do factor de necrose tumoral.
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
CN100376567C (zh) 1999-11-05 2008-03-26 阿斯特拉曾尼卡有限公司 作为vegf抑制剂的喹唑啉衍生物
GB9927191D0 (en) 1999-11-17 2000-01-12 Angeletti P Ist Richerche Bio Methods and means for regulation of gene expression
US7220552B1 (en) 1999-11-19 2007-05-22 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
AU1776501A (en) 1999-11-19 2001-05-30 Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and their use in the disruption of protein-protein interactions
DK1233943T3 (da) 1999-11-24 2011-08-15 Sugen Inc Ioniserbare indolinon derivater og anvendelse deraf som PTK ligander
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
US7141660B2 (en) 2000-02-08 2006-11-28 Sinvent As Genes encoding a nystatin polyketide synthase and their manipulation and utility
US6797514B2 (en) 2000-02-24 2004-09-28 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
US7572631B2 (en) 2000-02-24 2009-08-11 Invitrogen Corporation Activation and expansion of T cells
US6867041B2 (en) 2000-02-24 2005-03-15 Xcyte Therapies, Inc. Simultaneous stimulation and concentration of cells
BR0108545A (pt) 2000-02-24 2004-06-29 Xcyte Therapies Inc Estimulação e concentração simultâneas das células
EP1259595B1 (de) 2000-02-25 2007-04-04 Immunex Corporation Integrin antagonisten
EP1283827A2 (de) 2000-05-23 2003-02-19 Vertex Pharmaceuticals Incorporated Caspase inhibitoren und deren verwendung
US7176037B2 (en) 2000-07-13 2007-02-13 The Scripps Research Institute Labeled peptides, proteins and antibodies and processes and intermediates useful for their preparation
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
ES2556946T3 (es) 2000-12-21 2016-01-21 Novartis Ag Pirimidinaminas como moduladores de la angiogénesis
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US20030153053A1 (en) 2001-08-06 2003-08-14 Ralph Reid Methods for altering polyketide synthase genes
US6809077B2 (en) 2001-10-12 2004-10-26 Enanta Pharmaceuticals, Inc. Cyclosporin analogs for the treatment of autoimmune diseases
US6987090B2 (en) 2002-05-09 2006-01-17 Lg Household & Health Care Ltd. Use of 3-position cyclosporin derivatives for hair growth
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7012065B2 (en) 2003-02-07 2006-03-14 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of immune disorders
EP1477563A3 (de) 2003-05-16 2004-11-24 Wyeth Klonierung von Streptomyces cyaneogriseus subsp.noncyanogenus Genen zur Biosynthese von Antibiotika und Verfahren zu ihrer Verwendung
AU2004244626A1 (en) 2003-05-23 2004-12-09 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services GITR ligand and GITR ligand-related molecules and antibodies and uses thereof
WO2005005434A1 (en) 2003-07-08 2005-01-20 Novartis Ag Use of rapamycin and rapamycin derivatives for the treatment of bone loss
EP1648900A4 (de) 2003-07-11 2010-02-10 Ariad Pharma Inc Phosphorhaltige makrocyclen
US20050048054A1 (en) 2003-07-11 2005-03-03 Shino Hanabuchi Lymphocytes; methods
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
TWI378923B (en) 2003-08-15 2012-12-11 Novartis Ag Pyrimidine derivatives
WO2005055808A2 (en) 2003-12-02 2005-06-23 Genzyme Corporation Compositions and methods to diagnose and treat lung cancer
US20080058431A1 (en) 2004-03-26 2008-03-06 Gen-Sheng Feng Modulators of Shp2 Tyrosine Phosphatase and Their Use in the Treatment of Body Weight Disorders
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
US20060002932A1 (en) 2004-06-04 2006-01-05 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
GEP20104906B (en) 2004-08-26 2010-02-25 Pfizer Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
CN101039952A (zh) 2004-10-13 2007-09-19 惠氏公司 作为pi3k抑制剂的17－羟基渥曼青霉素类似物
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
PL2161336T5 (pl) 2005-05-09 2017-10-31 Ono Pharmaceutical Co Ludzkie przeciwciała monoklonalne przeciwko białku Programmed Death 1 (PD-1) oraz sposoby leczenia raka z zastosowaniem samych przeciwciał anty-PD-1 lub w połączeniu z innymi środkami immunoterapeutycznymi
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2622870A1 (en) 2005-09-20 2007-03-29 Pfizer Products Inc. Dosage forms and methods of treatment using a tyrosine kinase inhibitor
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
JP2009528292A (ja) 2006-02-27 2009-08-06 ザ ボード オブ トラスティーズ オブ レランド スタンフォード ジュニア ユニバーシティ 生物学的障壁を越える増強された放出特性を有する分子の輸送のための組成物および方法
US20070203168A1 (en) 2006-02-28 2007-08-30 Zhao Jonathon Z Isomers of rapamycin and 42-Epi-rapamycin, methods of making and using the same
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
WO2008070740A1 (en) 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
WO2008124815A1 (en) 2007-04-10 2008-10-16 University Of South Florida Method of activating nk cells
CN101801413A (zh) 2007-07-12 2010-08-11 托勒克斯股份有限公司 采用gitr结合分子的联合疗法
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
WO2009049098A2 (en) 2007-10-09 2009-04-16 Indiana University Research & Technology Corporation Materials and methods for regulating the activity of phosphatases
KR100945483B1 (ko) 2007-10-25 2010-03-05 이화여자대학교 산학협력단 ｐｉｋＤ 조절유전자의 발현벡터를 이용한 스트렙토미세스베네주엘라에（Ｓｔｒｅｐｔｏｍｙｃｅｓｖｅｎｅｚｕｅｌａｅ）에서폴리케타이드（ｐｏｌｙｋｅｔｉｄｅ）의 생산성 증가방법
EP2214675B1 (de) 2007-10-25 2013-11-20 Genentech, Inc. Verfahren zur herstellung von thienopyrimidin-verbindungen
GB0805363D0 (en) 2008-03-20 2008-04-30 Sinvent As Novel NRPS-PKS gene cluster and its manipulation and utility
WO2009135000A2 (en) 2008-04-30 2009-11-05 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-117199 and analogs
KR20110044992A (ko) 2008-07-02 2011-05-03 이머전트 프로덕트 디벨롭먼트 시애틀, 엘엘씨 ＴＧＦ-β 길항제 다중-표적 결합 단백질
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
CN102149820B (zh) 2008-09-12 2014-07-23 国立大学法人三重大学 能够表达外源gitr配体的细胞
EP2352526A1 (de) 2008-09-19 2011-08-10 Protox Therapeutics Inc. Behandlung von krebsstammzellen mithilfe gezielter transportproteine
US8962329B2 (en) 2008-09-24 2015-02-24 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Gene cluster
SG173180A1 (en) 2009-01-30 2011-09-29 Enanta Pharm Inc Cyclosporin analogues for preventing or treating hepatitis c infection
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
BR112012000867A2 (pt) 2009-07-13 2019-09-24 Harvard College "polipeptídeos bifuncional costurado e uso do mesmo"
US8664186B2 (en) 2009-07-24 2014-03-04 Universite De Lorraine Stambomycin and derivatives, their production and their uses as drugs
NZ598262A (en) 2009-08-17 2014-05-30 Sloan Kettering Inst Cancer Heat shock protein binding compounds, compositions, and methods for making and using same
PT3023438T (pt) 2009-09-03 2020-05-08 Merck Sharp & Dohme Anticorpos anti-gitr
JP2013505300A (ja) 2009-09-22 2013-02-14 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
EP2492344B1 (de) 2009-10-22 2016-04-06 PeptiDream Inc. Schnelles anzeigeverfahren bei der translationssynthese von peptiden
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
SI2519543T1 (sl) 2009-12-29 2016-08-31 Emergent Product Development Seattle, Llc Beljakovine, ki se vežejo s heterodimeri in njihova uporaba
US8637684B2 (en) 2010-05-12 2014-01-28 Wisconsin Alumni Research Foundation Tautomycetin and tautomycetin analog biosynthesis
WO2012041524A1 (en) 2010-10-01 2012-04-05 Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors
EP3287458B1 (de) 2010-11-30 2022-07-13 The Johns Hopkins University Zyklische hybride bibliotheken und screening dafür
PY1153144A (es) 2010-12-10 2015-01-01 Gilead Sciences Inc Inhibidores macrocíclicos de virus flaviviridae
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
DK2937349T3 (en) 2011-03-23 2017-02-20 Amgen Inc CONDENSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3
JP5997763B2 (ja) 2011-05-19 2016-09-28 フンダシオン セントロ ナシオナル デ インベスティガシオネス オンコロヒカス カルロス ザ サードＦｕｎｄａｃｉｏｎ Ｃｅｎｔｒｏ Ｎａｃｉｏｎａｌ ｄｅ Ｉｎｖｅｓｔｉｇａｃｉｏｎｅｓ Ｏｎｃｏｌｏｇｉｃａｓ Ｃａｒｌｏｓ ＩＩＩ タンパク質キナーゼ阻害剤としての大環状化合物
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
DE102011111991A1 (de) 2011-08-30 2013-02-28 Lead Discovery Center Gmbh Neue Cyclosporin-Derivate
WO2013039954A1 (en) 2011-09-14 2013-03-21 Sanofi Anti-gitr antibodies
CN104379563B (zh) 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
WO2013185090A1 (en) * 2012-06-08 2013-12-12 Gilead Sciences, Inc. Macrocyclic inhibitors of flaviviridae viruses
WO2013185103A1 (en) 2012-06-08 2013-12-12 Gilead Sciences, Inc. Macrocyclic inhibitors of flaviviridae viruses
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
EP3210627B1 (de) 2012-07-12 2022-12-21 Hangzhou Dac Biotech Co., Ltd Konjugate aus zellbindungsmolekülen mit zytotoxika
AU2012395148B2 (en) 2012-11-24 2016-10-27 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
BR112015021134A2 (pt) 2013-03-15 2017-10-10 Novartis Ag conjugados de fármaco e anticorpo
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)
EP2806274A1 (de) 2013-05-24 2014-11-26 AIT Austrian Institute of Technology GmbH Lungenkrebsdiagnoseverfahren und -mittel
CA2953482A1 (en) 2013-07-03 2015-01-08 Indiana University Research & Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
EP2826586A1 (de) 2013-07-18 2015-01-21 Siemens Aktiengesellschaft Verfahren und System zur Bearbeitung eines Objekts
JP6559123B2 (ja) 2013-10-10 2019-08-14 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの阻害剤
EP3094629B1 (de) 2014-01-17 2018-08-22 Novartis AG 1-(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idin-derivate und zusammensetzungen davon zur hemmung der aktivität von shp2
EP3094627B1 (de) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-(triazin-3-yl-piper(-azin)/idin/pyrolidin-derivate und zusammensetzungen daraus zur hemmung der aktivität von shp2
US10233431B2 (en) 2014-02-26 2019-03-19 The Regents Of The University Of California Producing 3-hydroxycarboxylic acid and ketone using polyketide synthases
EP3114483A1 (de) 2014-03-03 2017-01-11 Yissum Research and Development Company of the Hebrew University of Jerusalem Ltd. Verfahren und vorrichtung für den nachweis von pseudomonas aeruginosa
JO3474B1 (ar) * 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
TW201629069A (zh) 2015-01-09 2016-08-16 霍普驅動生物科技股份有限公司 參與協同結合之化合物及其用途
EP4289950A3 (de) 2015-01-09 2024-01-24 Revolution Medicines, Inc. Makrozyklische verbindungen mit beteiligung an einer kooperativen bindung und medizinische verwendungen davon
US10077289B2 (en) 2015-03-31 2018-09-18 Allergan, Inc. Cyclosporins modified on the MeBmt sidechain by heterocyclic rings
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (de) 2015-04-15 2020-12-02 Araxes Pharma LLC Kondensierte tricyclische inhibitoren von kras und anwendungsverfahren dafür
US20180121597A1 (en) 2015-05-22 2018-05-03 Allosta Pharmaceuticals Methods to Prepare and Employ Binding Site Models for Modulation of Phosphatase Activity and Selectivity Determination
US10532977B2 (en) 2015-06-01 2020-01-14 Indiana University Research And Technology Corporation Small molecule inhibitors of protein tyrosine phosphatases and uses thereof
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2017015562A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
EP3356354A1 (de) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (de) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
EP3356347A1 (de) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
EP3356349A1 (de) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
EP3355930A4 (de) 2015-10-01 2019-03-06 Warp Drive Bio, Inc. Verfahren und reagenzien zur analyse von protein-protein-schnittstellen
WO2017078499A2 (ko) 2015-11-06 2017-05-11 경북대학교 산학협력단 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물
WO2017079723A1 (en) 2015-11-07 2017-05-11 Board Of Regents, The University Of Texas System Targeting proteins for degradation
EP3377481A1 (de) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituierte chinazolinverbindungen mit einer substituierten heterocyclischen gruppe und verfahren zur verwendung davon
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US9932288B2 (en) 2015-12-09 2018-04-03 West Virginia University Chemical compound for inhibition of SHP2 function and for use as an anti-cancer agent
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
CN109843856B (zh) 2016-05-18 2023-05-02 米拉蒂治疗股份有限公司 Kras g12c抑制剂
JP7044375B2 (ja) 2016-05-31 2022-03-30 ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム Ｐｔｐｎ１１の複素環式阻害剤
EA202092442A3 (ru) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
EP3519402A1 (de) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
WO2018081592A2 (en) 2016-10-28 2018-05-03 Warp Drive Bio, Inc. Compositions and methods for the production of compounds
CA3043131A1 (en) 2016-11-18 2018-05-24 Neurovive Pharmaceutical Ab Use of sanglifehrin macrocyclic analogues as anticancer compounds
EP3555077B1 (de) 2016-12-15 2023-04-19 The Regents of The University of California Zusammensetzungen und verfahren zur behandlung von krebs
CA3048217A1 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
WO2018129402A1 (en) 2017-01-06 2018-07-12 Oregon Health & Science University Compositions and methods used in diagnosing and treating colorectal cancer
EP3568204B1 (de) 2017-01-10 2023-08-30 Novartis AG Pharmazeutische kombination mit einem alk-inhibitor und einem sp2-inhibitor
SG11201906412SA (en) 2017-01-23 2019-08-27 Revolution Medicines Inc Pyridine compounds as allosteric shp2 inhibitors
BR112019015075A2 (pt) 2017-01-23 2020-03-10 Revolution Medicines, Inc. Compostos bicíclicos como inibidores de shp2 alostéricos
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573966A1 (de) 2017-01-26 2019-12-04 Araxes Pharma LLC Kondensierte heterocyclische verbindungen und verfahren zur verwendung davon
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (de) 2017-01-26 2019-12-04 Araxes Pharma LLC Fusionierte bicyclische benzoheteroaromatische verbindungen und verfahren zur verwendung davon
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
US20200048359A1 (en) 2017-02-28 2020-02-13 Novartis Ag Shp inhibitor compositions and uses for chimeric antigen receptor therapy
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
IL269779B2 (en) 2017-04-05 2026-04-01 Revolution Medicines Inc Methods and reagents for the analysis of protein-protein interfaces
KR20200003803A (ko) 2017-04-05 2020-01-10 레볼루션 메디슨즈, 인크. 협동 결합에 참여하는 화합물 및 그의 용도
IL303660A (en) 2017-05-02 2023-08-01 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors
AU2018264511A1 (en) * 2017-05-09 2019-11-07 Eisai R&D Management Co., Ltd. Therapeutic agent containing pyranodipyridine compound
AR111776A1 (es) 2017-05-11 2019-08-21 Astrazeneca Ab Heteroarilos inhibidores de las proteínas ras mutantes de g12c
ES2905676T3 (es) 2017-05-22 2022-04-11 Amgen Inc Inhibidores de KRAS G12C y métodos para su uso
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
JP7356414B2 (ja) 2017-09-07 2023-10-04 レヴォリューション・メディスンズ，インコーポレイテッド がんを治療するためのｓｈｐ２阻害剤組成物および方法
CN111051306B (zh) 2017-09-08 2023-01-03 美国安进公司 Kras g12c的抑制剂及其使用方法
CN118684652A (zh) 2017-09-11 2024-09-24 克鲁松制药公司 SHP2的八氢环戊二烯并[c]吡咯别构抑制剂
KR102861303B1 (ko) 2017-11-15 2025-09-17 미라티 테라퓨틱스, 인크. Ｋｒａｓ ｇ12ｃ 억제제
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
CA3098698A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
CN118978535A (zh) 2018-05-01 2024-11-19 锐新医药公司 作为mTOR抑制剂的C40-、C28-及C-32连接的雷帕霉素类似物
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
EP3790886B1 (de) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c-inhibitoren zur behandlung von krebs
AU2019278998B2 (en) 2018-06-01 2023-11-09 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
CR20210083A (es) 2018-08-16 2021-04-19 Hoffmann La Roche Compuestos de anillo fusionado
US20210230170A1 (en) 2018-08-31 2021-07-29 Mirati Therapeutics, Inc. Kras g12c inhibitors
CA3117222A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CN113498342A (zh) * 2018-12-21 2021-10-12 锐新医药公司 参与协同结合的化合物和其用途
PE20221277A1 (es) 2019-11-04 2022-09-05 Revolution Medicines Inc Inhibidores de ras
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
AU2021345111B2 (en) 2020-09-15 2025-11-27 Revolution Medicines, Inc. Indole derivatives as Ras inhibitors in the treatment of cancer

Also Published As

Publication number Publication date
CN120699039A (zh) 2025-09-26
WO2021091967A1 (en) 2021-05-14
BR112022008534A2 (pt) 2022-08-09
CR20220240A (es) 2022-08-03
US11739074B2 (en) 2023-08-29
AU2025210782A1 (en) 2025-08-21
IL292642A (en) 2022-07-01
CN121471132A (zh) 2026-02-06
CL2025000457A1 (es) 2025-06-23
CA3159559A1 (en) 2021-05-14
MX2022005357A (es) 2022-06-02
CL2023000973A1 (es) 2023-09-29
CO2022006030A2 (es) 2022-07-29
EP4656201A2 (de) 2025-12-03
EP4656201A3 (de) 2025-12-17
EP4054720A1 (de) 2022-09-14
KR20250133996A (ko) 2025-09-09
IL322454A (en) 2025-09-01
CN115873020A (zh) 2023-03-31
JP7823816B2 (ja) 2026-03-04
TW202132315A (zh) 2021-09-01
CN114901366A (zh) 2022-08-12
JP2022553857A (ja) 2022-12-26
PH12022550973A1 (en) 2023-09-25
IL292642B1 (en) 2026-04-01
PE20221277A1 (es) 2022-09-05
AU2020379731A1 (en) 2022-05-05
CN115873020B (zh) 2025-06-13
US20250051306A1 (en) 2025-02-13
US20210130326A1 (en) 2021-05-06

Similar Documents

Publication Publication Date Title
JP7823816B2 (ja) Ｒａｓ阻害剤
JP7789906B2 (ja) Ｒａｓ阻害剤
EP4054719B1 (de) Ras-inhibitoren
KR20240004960A (ko) Ras 억제제
KR20240132492A (ko) Ras 억제제
AU2022268962A1 (en) Ras inhibitors for the treatment of cancer
KR20220109407A (ko) Ras 억제제
WO2022060836A1 (en) Indole derivatives as ras inhibitors in the treatment of cancer
JP2025521232A (ja) 大環状ｒａｓ阻害剤
KR20260005904A (ko) 매크로사이클릭 ras 억제제
HK40128485A (en) Ras inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

A16 Divisional, continuation or continuation in part application filed

Free format text: ST27 STATUS EVENT CODE: A-0-1-A10-A16-DIV-PA0104 (AS PROVIDED BY THE NATIONAL OFFICE)

PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A16-div-PA0104

D21 Rejection of application intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11 Administrative time limit extension requested

Free format text: ST27 STATUS EVENT CODE: U-3-3-T10-T11-OTH-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11 Administrative time limit extension requested

Free format text: ST27 STATUS EVENT CODE: U-3-3-T10-T11-OTH-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13 Pre-grant limitation requested

Free format text: ST27 STATUS EVENT CODE: A-2-3-E10-E13-LIM-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000